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Publication numberUS4895676 A
Publication typeGrant
Application numberUS 07/296,275
Publication date23 Jan 1990
Filing date11 Jan 1989
Priority date1 Aug 1986
Fee statusPaid
Also published asCA1304196C, DE255967T1, DE3775853D1, EP0255967A1, EP0255967B1, US5013484
Publication number07296275, 296275, US 4895676 A, US 4895676A, US-A-4895676, US4895676 A, US4895676A
InventorsMauro De Gregorio
Original AssigneeAziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A.
Export CitationBiBTeX, EndNote, RefMan
External Links: USPTO, USPTO Assignment, Espacenet
Bendazac or 5-hydroxy derivative
US 4895676 A
Abstract
Treatment of contact lenses by an effective amount of bendazac, 5-hydroxybendazac or a salt thereof with a physiologically acceptable base.
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Claims(12)
What is claimed is:
1. A method of inhibiting protein sedimentation from Lacrimal fluid on a contact lens and neutralizing irritative effect of existing protein sediments without substantially affecting mucus secretion by mucous membranes of the contact leans wearer wherein said lens is contacted with an effective amount of a composition comprising bendazac, 5-hydroxy-bendazac, or a salt thereof with an inorganic or organic physiologically acceptable base, and a physiologically acceptable carrier said contact occurring prior to insertion into the eye.
2. The method, as in claim 1 wherein the contact lens is a soft contact lens.
3. The method, as in claim 1 wherein the effective amount of bendazac or 5-hydroxy-bendazac is 0.05-2% or the corresponding amount of the salt thereof.
4. The method, as in claim 1 wherein the physiologically acceptable base is selected from the group consisting of sodium, potassium, aliphatic amines and basic aminoacids.
5. The method, as in claim 1 wherein the polysiologically acceptable carrier is water.
6. The method, as in claim 1 wherein the composition further comprises surfactants or enzymes.
7. The method, as in claim 1 wherein the composition further comprises one or more of the group consisting of preservatives, salts for regulating osmotic pressure, antiseptics disinfectants, antioxidants and buffers.
8. The method, as in claim 1 wherein the contact lens is contacted with the composition for at least one hour.
9. The method, as in claim 6 wherein the enzyme comprises papain.
10. The method, as in claim 6 wherein the surfactant comprises octylphenyoryoctanol.
11. The method, as in claim 7 wherein the disinfectant comprises chlorhexidine gluconate.
12. The method, as in claim 1 wherein the composition comprises, in 100 mls of distilled water
______________________________________Bendazac lysinate      0.4     gHydroxy ethyl cellulose                  0.4     gPolyvinyl alcohol      1.4     gThymerosal             0.004   gSodium edetate         0.2     gSodium chloride        0.75    gBoric acid or borax to pH 7.4.______________________________________
Description

This is a continuation of co-pending application Ser. No. 077,620 filed on July 24, 1987, now abandoned.

This invention relates to a method of treating contact lenses.

More particularly, it relates to the use of compound which inhibit proteins sedimentation from lacrimal fluid on contact lenses, preferably of the soft type, and neutralize possible protein sediments without substantially affecting mucus secretion by mucous membranes.

It is known that soft contact lenses represent a progress in comparison with rigid ones in that they do not cause and do not transmit mechanical traumas to the eye. Nevertheless, they have the drawback of quickly undergoing opaqueness because of protein sediments from lacrimal fluid, the amount and nature of which are widely different from individual to individual. Moreover, very often, the said protein sediments promote a keratoconjuctival process of sensitization which causes corneal irritation phenomena.

Several washing techniques have been suggested for removing the above said sediments, preferably by means of solutions containing surfactants or enzymes.

These techniques, however, do not allow removing all the sediments and leave some residue which causes the above mentioned drawbacks.

Therefore, a compound is still in great demand capable of completely, or to a great extent, preventing the formation of protein sediments on contact lenses and which anyhow is capable of preventing the small sediment, so formed, from having sensitization properties.

It has been now found that the so called "Aspirin-like" compounds, that is the non-steroid antiinflammatory acid compounds, such as salicylic acid, phenylbutazone, ibuprofen and mefenamic acid, posses such properties.

These compounds, however, substantially reduce the amount of mucus secreted by mucous membranes. Since mucus plays a very important role in protecting the eye, the so called "Aspirin-like" compounds result to be contraindicated for contacting the eye.

Furthermore, it has been now surprisingly found that bendazac, 5-hydroxy-bendazac and their salts with inorganic or organic physiologically acceptable bases, inhibit sedimentation of proteins from lacrimal fluid on contact lenses and neutralize the irritative properties of possible protein sediments without substantially affecting the secretion of mucus by mucous membranes.

It is, therefore, an object of this invention to provide a method of treating contact lenses, preferably of the soft type, comprising contacting a lens with an effective amount of bendazac, 5-hydroxy-bendazac or salt thereof with an organic or inorganic physiologically base.

The compounds of formula: ##STR1## where R is H (bendazac) or OH (5-hydroxy-bendazac), and their salts with inorganic and organic physiologically acceptable bases, are already known, for example from the Italian patent application Nr. 49,790 A/81 of Nov. 27, 1981 and European patent application Nr. 191,520 of Jan. 29, 1986 that describe their use as anticataract agents.

Examples of suitable bases are the alkali metals such as sodium and potassium, the aliphatic amines, the basic aminoacids such as lysine and arginine, and the like.

Before being contacted with the lens, a compound of formula I or a physiologically acceptable salt thereof is preferably dissolved into a liquid.

The contact time of the solution comprising a compound of formula I or a physiologically acceptable salt thereof with a lens shall, of course, vary depending on the compound and the type of solution used. For instance, such time will be at least one hour in the case of deterging or wetting solutions, whereas it will be a few minutes in the case of rinsing solutions.

Another object of this invention is to provide the use of a compound of formula I or of a physiologically acceptable salt thereof for preparing solutions for the treatment of contact lenses.

The said solutions are prepared by dissolving a compound of formula I or a physiologically acceptable salt thereof in a non-toxic solvent which is compatible with both the said compound and the lens and which is suitable for undergoing sterilization. Preferably, the said solvent consists of purified or distilled sterile water.

The solutions of this invention may also comprise other ingredients, the nature and amount of which vary depending on the type of solution to be prepared; this may indeed be of a wetting, deterging, disinfecting or rinsing type.

In the case of individuals in which the compound of formula I used or its physiologically acceptable salt is not capable of inhibiting up to 100% of the formation of protein sediments, the solutions prepared according to this invention are used together with solutions comprising surfactants or enzymes, or they themselves comprise surfactants and/or enzymes. However the time before the lens becomes opaque is much longer in the case of the lens thus treated than that observed, for the same individual, when the lens is treated with surfactants and/or enzymes alone and even the probability of the arising of corneal irritation is very reduced compared to that of the usual treatments.

Examples of other suitable ingredients are preservatives, salts for regulating the osmotic pressure, antiseptics, disinfectants, antioxidants and buffers.

Said solutions may be easily prepared according to usual techniques which are well known to the people skilled in this art and comprise simple operations such as dissolving and sterilization.

A further object of this invention is to provide aqueous solutions comprising an effective amount of a compound of formula I or of a physiologically acceptable salt thereof, which are suitable for wetting, deterging or rinsing contact lenses.

Typical examples of solutions according to this invention comprise a compound of formula I or a physiologically acceptable salt thereof and at least a disinfectant, a surfactant and/or an enzyme.

Examples of suitable disinfectants, surfactants and enzymes are chlorhexidine gluconate, octylphenoxyoctanol and papain, respectively.

Preferably the solutions according to this invention comprise from 0.05 to 2% of bendazac, or of 5-hydroxy-bendazac, or the corresponding amount of a salt with a physiologically acceptable organic or inorganic base.

The following examples are given to illustrate this invention without, however, limiting it in any way.

EXAMPLE 1

______________________________________Wetting solution100 ml contain:______________________________________Bendazac sodium salt              0.25        gHydroxy ethyl cellulose              0.4         gPolyvinyl alcohol  1.4         gThymerosal         0.004       gSodium edetate     0.20        gSodium chloride    0.75        gBoric acid or borax to              pH 7.4Sterile distilled water q.s. to              100         ml______________________________________
EXAMPLE 2

______________________________________Wetting solution100 ml contain:______________________________________5-hydroxybendazac  0.25        gHydroxy ethyl cellulose              0.4         gPolyvinlyl alcohol 1.4         gThymerosal         0.004       gSodium edetate     0.20        gSodium chloride    0.65        gAnhydrous Sodium sulfite              0.15        g1 N Sodium hydroxide to              pH 6.5Sterile distilled water q.s. to              100         ml______________________________________
EXAMPLE 3

______________________________________Deterging solution100 ml contain:______________________________________Bendazac sodium salt              0.25        gPolivinyl alchol   1.4         gThymerosal         0.004       gSodium edetate     0.20        gSodium chloride    0.75        gOctyl phenoxy ethanol              0.35        gBoric acid or borax to              pH 7.4Sterile distilled water q.s. to              100         ml______________________________________
EXAMPLE 4

______________________________________Deterging solution100 ml contain:______________________________________5-hydroxybendazac       0.25    gPolyvinyl alcohol       1.4     gThymerosal              0.004   gSodium edetate          0.20    gSodium chloride         0.65    gAnhydrous Sodium sulfite                   0.15    gOctyl phenoxy ethanol   0.35    g1 N Sodium hydroxide to pH 6.5Sterile distilled water q.s. to                   100     ml______________________________________
EXAMPLE 5

______________________________________Disinfecting solution100 ml contain:______________________________________Bendazac sodium salt    0.25    gSodium chloride         0.75    gThymerosal              0.001   gChlohrexidine gluconate 0.005   gSodium edetate          0.1     gPolysorbate 80          0.05    gBoric acid or borax to  pH 7.4Sterile demineralized water q.s. to                   100     ml______________________________________
EXAMPLE 6

______________________________________Disinfecting solution100 ml contain:______________________________________5-hydroxybendazac        0.25   gSodium chloride          0.65   gAnhydrous Sodium sulfite 0.15   gThymerosal               0.001  gChlorhexidine gluconate  0.005  gSodium edetate           0.1    gPolysorbate 80           0.05   gSterile demineralized water q.s. to                    100    ml______________________________________
EXAMPLE 7

______________________________________Solution for rinsing or thermal disinfection100 ml contain:______________________________________Bendazac                0.25    gSodium chloride         0.75    gThymerosal              0.001   gSodium edetate          0.1     gBoric acid or borax to  pH 7.4Sterile demineralized water q.s. to                   100     ml______________________________________
EXAMPLE 8

______________________________________Solution for rinsing or thermal disinfection100 ml contain:______________________________________5-hydroxybendazac       0.25    gSodium chloride         0.65    gAnhydrous Sodium sulfite                   0.15    gThymerosal              0.001   gSodium edetate          0.1     g1 N Sodium hydroxide to pH 6.5Sterile demineralized water q.s. to                   100     ml______________________________________
EXAMPLE 9

______________________________________Wetting solution100 ml contain:______________________________________Bendazac lysinate  0.4         gHydroxy ethyl cellulose              0.4         gPolyvinyl alcohol  1.4         gThymerosal         0.004       gSodium edetate     0.2         gSodium chloride    0.75        gBoric acid or borax to              pH 7.4Sterile distilled water q.s. to              100         ml______________________________________

A first experiment has been carried out on six individuals wearing soft contact lenses and specifically selected because they produced every 5-6 days such an amount of sediments on the said lenses that they had to treat their lenses daily with a deterging composition containing a surfactant, and weekly with a composition containing a proteolytic enzyme.

These individuals stopped using the composition containing a proteolytic enzyme. For a period of three months they regularly dipped their lenses in a solution according to example 9 every night after the usual deterging and disinfecting treatment. More particularly, the lenses were kept in the above solution overnight.

In the course of the entire three months period, all six individuals did not need to clean their lenses with any composition containing a proteolytic enzyme.

A second experiment has been carried out on ten individuals whose soft contact lenses showed appreciable sediments easily detectable, observing the lenses on a black background through a 7-fold magnification. These individuals used the solution according to example 8 by contacting directly the worn lenses in situ with two drops of the said solution 4 times a day.

The regular use of the said solution for 14 consecutive days caused, in all ten individuals, disappearance or substantial reduction of the sediments on the lenses.

Patent Citations
Cited PatentFiling datePublication dateApplicantTitle
US4451477 *8 Jun 198229 May 1984Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A.Bendazac treatment of cataract
EP0191520A1 *29 Jan 198620 Aug 1986AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.(1-phenylmethyl-5-hydroxy-1H-indazol-3-yl)-oxyacetic acid and salts thereof for use as a medicament, and pharmaceutical compositions containing them
Referenced by
Citing PatentFiling datePublication dateApplicantTitle
US5277708 *19 Jan 199311 Jan 1994S&S Industrial Services, Inc.Alkaline, water washable mixture comprising fatty acids and fatty esters, grit, water, acrylic copolymer
US5451237 *10 Nov 199319 Sep 1995Vehige; Joseph G.Antideposit agents for proteins on contact lenses with FD&C green 3 and methylene blue
Classifications
U.S. Classification106/2, 8/507, 134/42, 510/490, 510/114, 510/112, 514/407, 510/386, 510/393, 514/839
International ClassificationC07D231/56, A61K31/415, A61L12/14, G02C13/00, A61L2/18, G02C7/04, A61L2/16
Cooperative ClassificationY10S514/912, Y10S514/839, A61L12/146
European ClassificationA61L12/14F
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